title: Synthesis of 6-amino-6-deoxyhyaluronan as an intermediate for conjugation with carboxylate-containing compounds: application to hyaluronan-camptothecin conjugates.
abstract: A novel methodology for making drug conjugates using hyaluronan as a carrier was developed. This strategy involves a completely regioselective two-step synthesis of 6-amino-6-deoxyhyaluronan, which is then easily functionalized with drugs through a suitable linker. The case of hyaluronan-camptothecin conjugates is described, making use of a simple succinate linker. The antitumor activity of new hyaluronan derivatives prepared is at present under evaluation.
authors.affiliation: Eurand S.p.A., Area Science Park, Padriciano 99, 34012 Trieste, Italy. stefano.norbedo@eurand.com
authors.forename: Stefano
authors.initials: S
authors.lastname: Norbedo
authors.forename: Francesca
authors.initials: F
authors.lastname: Dinon
authors.forename: Massimo
authors.initials: M
authors.lastname: Bergamin
authors.forename: Susanna
authors.initials: S
authors.lastname: Bosi
authors.forename: Vincent
authors.initials: V
authors.lastname: Aroulmoji
authors.forename: Riaz
authors.initials: R
authors.lastname: Khan
authors.forename: Erminio
authors.initials: E
authors.lastname: Murano
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry*; D002166:Camptothecin / Q000737:chemistry*; D002264:Carboxylic Acids / Q000737:chemistry*; D006820:Hyaluronic Acid / Q000737:chemistry*; D015394:Molecular Structure; D013237:Stereoisomerism
chemical_list: D000970:Antineoplastic Agents; D002264:Carboxylic Acids; D006820:Hyaluronic Acid; D002166:Camptothecin